2. Academic Validation
  3. Investigation of the effect of structure modification of furamidine on the DNA minor groove binding and antiprotozoal activity

Investigation of the effect of structure modification of furamidine on the DNA minor groove binding and antiprotozoal activity

  • Eur J Med Chem. 2023 Apr 5:252:115287. doi: 10.1016/j.ejmech.2023.115287.
Abdelbasset A Farahat 1,  Arvind Kumar 2,  Tanja Wenzler 3,  Reto Brun 3,  Ananya Paul 2,  Pu Guo 2,  W David Wilson 2,  David W Boykin 2
Affiliations

Affiliations

  • 1 Masters of Pharmaceutical Sciences Program, California Northstate University, Elk Grove, CA, 95757, USA; Department of Pharmaceutical Organic Chemistry, Faculty of Pharmacy, Mansoura University, Mansoura, 35516, Egypt. Electronic address: abdelbasset.farahat@cnsu.edu.
  • 2 Department of Chemistry, Georgia State University, Atlanta, GA, 30303, USA.
  • 3 Swiss Tropical and Public Health Institute, Basel, 4002, Switzerland; University of Basel, Basel, 4003, Switzerland.
PMID: 36958267 DOI: 10.1016/j.ejmech.2023.115287
Abstract

New analogs of the antiprotozoal agent Furamidine were prepared utilizing Stille coupling reactions and amidation of the bisnitrile intermediate using lithium bis-trimethylsilylamide. Both the phenyl groups and the furan moiety of furamidine were replaced by heterocycles including thiophene, selenophene, indole or benzimidazole. Based upon the ΔTm and the CD results, the new compounds showed strong binding to the DNA minor groove. The new analogues are also more active both in vitro and in vivo than furamidine. Compounds 7a, 7b, and 7f showed the highest activity in vivo by curing 75% of Animals, and this merits further evaluation.

Keywords

Amidines; Antimalarial; Antitrypanosomal; DNA minor Groove binders; Lithium bis(trimethylsilyl)amide; Stille coupling.

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